Description
As a novel inhibitor, nepicastat hydrochloride can potently inhibit bovine and human dopamine-beta-hydroxylase with IC50 of 8.5 nM and 9 nM. respectively.
Storage
2 years at -20 centigrade
Targets
bovine dopamine-beta-hydroxylase, human dopamine-beta-hydroxylase
Molecular Formula
C14H15F2N3S.HCl
Chemical Name
(S)-5-(aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1H-imidazole-2(3H)-thione hydrochloride
Solubility
DSMO 66 mg/mL Water
In vitro
Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM.
In vivo
In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produces the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%).
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